AU2009329493B2 - Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders - Google Patents

Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders Download PDF

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Publication number
AU2009329493B2
AU2009329493B2 AU2009329493A AU2009329493A AU2009329493B2 AU 2009329493 B2 AU2009329493 B2 AU 2009329493B2 AU 2009329493 A AU2009329493 A AU 2009329493A AU 2009329493 A AU2009329493 A AU 2009329493A AU 2009329493 B2 AU2009329493 B2 AU 2009329493B2
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Australia
Prior art keywords
factor
protein
seq
chimeric
derivative
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Ceased
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AU2009329493A
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AU2009329493A1 (en
Inventor
Ghislaine Cherel
Olivier Christophe
Cecile Denis
Paul Gueguen
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Institut National de la Sante et de la Recherche Medicale INSERM
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Institut National de la Sante et de la Recherche Medicale INSERM
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Priority claimed from EP08305990A external-priority patent/EP2199387A1/en
Application filed by Institut National de la Sante et de la Recherche Medicale INSERM filed Critical Institut National de la Sante et de la Recherche Medicale INSERM
Publication of AU2009329493A1 publication Critical patent/AU2009329493A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745Blood coagulation or fibrinolysis factors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K19/00Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • C12N9/48Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • C12N9/48Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424Serine endopeptidases (3.4.21)
    • C12N9/6429Thrombin (3.4.21.5)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • C12N9/48Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424Serine endopeptidases (3.4.21)
    • C12N9/6432Coagulation factor Xa (3.4.21.6)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • C12N9/48Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424Serine endopeptidases (3.4.21)
    • C12N9/6464Protein C (3.4.21.69)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y304/00Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21Serine endopeptidases (3.4.21)
    • C12Y304/21005Thrombin (3.4.21.5)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y304/00Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21Serine endopeptidases (3.4.21)
    • C12Y304/21006Coagulation factor Xa (3.4.21.6)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y304/00Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21Serine endopeptidases (3.4.21)
    • C12Y304/21069Protein C activated (3.4.21.69)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2319/00Fusion polypeptide

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2009329493A 2008-12-19 2009-12-21 Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders Ceased AU2009329493B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP08305990.7 2008-12-19
EP08305990A EP2199387A1 (en) 2008-12-19 2008-12-19 Serine protease derivatives and uses for the prevention and/or the treatment of blood coagulation disorders
EP09305349 2009-04-23
EP09305349.4 2009-04-23
US22296009P 2009-07-03 2009-07-03
US61/222960 2009-07-03
PCT/EP2009/067632 WO2010070137A1 (en) 2008-12-19 2009-12-21 Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders

Publications (2)

Publication Number Publication Date
AU2009329493A1 AU2009329493A1 (en) 2011-07-21
AU2009329493B2 true AU2009329493B2 (en) 2014-09-18

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009329493A Ceased AU2009329493B2 (en) 2008-12-19 2009-12-21 Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders

Country Status (9)

Country Link
US (3) US8436144B2 (zh)
EP (1) EP2358874B1 (zh)
JP (1) JP5833448B2 (zh)
KR (1) KR20110114587A (zh)
CN (2) CN102325880B (zh)
AU (1) AU2009329493B2 (zh)
CA (1) CA2747065A1 (zh)
ES (1) ES2629099T3 (zh)
WO (1) WO2010070137A1 (zh)

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* Cited by examiner, † Cited by third party
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MX2008006313A (es) * 2005-11-15 2008-11-06 Philadelphia Children Hospital Metodos y composiciones para modular la hemostasia.
PT2915564T (pt) 2007-09-28 2021-02-09 Alexion Pharma Inc Antídotos para inibidores do fator xa e métodos de utilização dos mesmos
US8455439B2 (en) 2008-11-14 2013-06-04 Portola Pharmaceuticals, Inc. Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents
JP5833448B2 (ja) * 2008-12-19 2015-12-16 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用
ES2607935T3 (es) 2009-03-30 2017-04-04 Portola Pharmaceuticals, Inc. Antídotos para inhibidores del factor Xa y procedimientos de uso de los mismos
WO2011008885A1 (en) 2009-07-15 2011-01-20 Portola Pharmaceuticals, Inc. Unit dose formulation of antidotes for factor xa inhibitors and methods of using the same
US9371522B2 (en) * 2011-09-30 2016-06-21 The Children's Hospital Of Philadelphia Compositions and methods for modulating hemostasis
IN2015DN01404A (zh) 2012-07-25 2015-07-03 Catalyst Biosciences Inc
ES2761730T3 (es) 2013-01-31 2020-05-20 Pfizer Composiciones y procedimientos para contrarrestar la inhibición del factor Xa
FR3001729B1 (fr) * 2013-02-04 2015-03-06 Lab Francais Du Fractionnement Mutants du facteur x
EP2970933A2 (en) * 2013-03-12 2016-01-20 Novo Nordisk A/S Thrombin sensitive coagulation factor x molecules
CN105579468A (zh) 2013-09-24 2016-05-11 辉瑞大药厂 包含重组人凝血因子Xa蛋白的异质性群体的组合物
US10676730B2 (en) 2015-01-07 2020-06-09 Inserm (Institut National De La Sante Et De La Recherche Medicale) Mutated factor X polypeptides and uses thereof for the treatment of haemophilia
US10655119B2 (en) 2015-07-25 2020-05-19 Inserm (Institut National De La Sante Et De La Recherche Medicale) Mutated factor X polypeptides and uses thereof for the treatment of haemophilia

Citations (1)

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WO2006018204A1 (en) * 2004-08-17 2006-02-23 Zlb Behring Gmbh Modified vitamin k dependent polypeptides

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Also Published As

Publication number Publication date
JP2012512645A (ja) 2012-06-07
AU2009329493A1 (en) 2011-07-21
US20130101570A1 (en) 2013-04-25
EP2358874A1 (en) 2011-08-24
CN102325880A (zh) 2012-01-18
US8518400B2 (en) 2013-08-27
JP5833448B2 (ja) 2015-12-16
CN104262479A (zh) 2015-01-07
WO2010070137A1 (en) 2010-06-24
CA2747065A1 (en) 2010-06-24
ES2629099T3 (es) 2017-08-07
KR20110114587A (ko) 2011-10-19
US20110293597A1 (en) 2011-12-01
US8436144B2 (en) 2013-05-07
EP2358874B1 (en) 2017-03-29
US8741286B2 (en) 2014-06-03
US20130261060A1 (en) 2013-10-03
CN102325880B (zh) 2014-10-01

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